Vaginal douche solution



United States Patent No Drawing. Continuation of application Ser. No. 9,688, Feb. 19, 1960. This application Jan. 16, 1963, Ser. No. 251,978

4 Claims. (Cl. 167-58) This application is a continuation of application Serial No. 9,688, filed February 19, 1960, which aplication has been abandoned.

While some gynecologists have long been critical of the vaginal douche, nevertheless, vaginal douching retains its popularity with women and is prescribed by many physicians including gynecologists, for various purposes. These include the treatment of vaginitis, either as the sole therapy or, more frequently, in conjunction with intravaginal instillations of medicated tablets, creams, or jellies. Douching is recommended in the routine of diaphragm contraception. In vaginal surgery, preoperative douching is a generally accepted procedure.

Such Widespread use in spite of authoritative criticism, is not paradoxical, but indicates that the vaginal douche has important positive values as well as serious shortcomings. Douching may serve a brief palliative purpose, temporarily removing by mechanical means the products of irritation, ulceration, or inflammation. This is, of course, the principal reason for employing a vaginal douche. Heretofore, a douche has not really cleansed properly for it failed to remove that which adheres to crevices resulting from vaginal rugosity. Furthermore, because of brevity of contact with the vaginal mucous, the fluid of the douche has not been a good medium for medication.

To enhance the mechanical cleansing of the vagina was the primary object of our investigation. But douching has further shortcomings. Douche nozzles are usually long, extending the entire length of the vagina, and cervical intromission of the douche fluid is possible. Few douche nozzles can be sterilized by boiling and none available hitherto can be autoclaved. Perhaps in a vain effort to overcome the defects, a quart and a half of fluid was used in the vaginal douche, an extraordinarily large quantity as compared, for example, with the amount used in a mouth wash. This necessitated lying down in a bathtub, and many homes that are equipped with bathtubs have tile walls into which it is not desirable to drive a nail in order to suspend the douche bag. This is important because the height of the bag regulates the douche-fluid pressure.

Finally, douching is a time-consuming and messy chore.

It is hence an object of this invention to provide a vaginal douche means which will overcome the objections noted above. This is achieved by providing douche means which will create an aerosol foam instilled in the vagina through the use of an inert propellant combined with an ingredient to achieve such a foam. The ingredient, according to the present invention, comprises a germicidal or antiseptic wetting agent or surface acting agent. The foam will hence cling and spread on the vaginal mucosa, that is, it will spread in between the rugae of the vagina and in the indentations and crevices.

There may also be combined with this ingredient, an ingredient which augments the first ingredient, the same comprising a wetting agent, and also being an emollient, having soothing properties helping to emulsify the first ingredient, and which will also help to hold Water. Also in the combination there is preferably employed an ingredient to lower the pH to encourage B. acidophiius growth.

Formulation Two surface-active ingredients have been combined to promote spreading of the solution on the vaginal mucosa, and to maintain active contact, and an inert, non-toxic aerosol propellant enhances the spreading action and penetrations of the solution into the crevices between the vaginal rugae.

One of the surface-active ingredients is cetyl-trimethylammonium bromide, C ,,H (CH NBr, a cationic quaternary detergent Which has bacteriocidal properties against both gram-positive and gram-negative organisms. Its phenol coeflicient for Staph. aureus is 250+. It is bacteriostatic, non-toxic and non-irritating even on raw surfaces, in the concentration employed in the present solution.

Two other quaternary detergents which may be used are dimethyl benzyl ammonium chloride and cetyl-trimethyl-ammonium iodine.

The second surface-active agent is a non-toxic ethoxylated fatty acid or alcohols such as ethoxylated lanolin alcohols. This aids in maintaining prolonged contact between the cetyl-trimethylammonium bromide and the vaginal mucosa. This mild surfactant is derived from sterols and fatty alcohols normally found in skin lipids and cellular tissues of epidermal origin. The persistent film is emollient and also holds moisture.

Two other non-ionics which may be used are ethoxylated alkyl phenols and ethoxylated sorbitol esters (for example polyoxyethylene sorbitan monolaurate).

To encourage growth of B. acidophilus (Doderleins bacillus), a pH of 5.0 is maintained by the addition of an organic acid such as lactic acid and buffering, such as with sodium bicarbonate.

Instead of lactic acid and its bulfering sodium bicarbonate or sodium lactate, there may also be used citric acid with sodium citrate or acetic acid with sodium acetate.

Tetratluoro-dichloro-ethane, an inert, non-toxic and non-reactive propellant was selected. It enters into physicochemical combination with the active ingredients and rapidly converts a small amount of fluid to a soft, voluminous foam. The expansion is persistent. It agitates the fluid, promoting continuous contact with the vaginal mucosa and its folds.

Another propellant that may be used is trichloromonofiuoromethane.

Tetralluoro-dichloro-ethane has a vapor pressure (absolute) of 27.5 p.s.i.a. at F., and 46 p.s.i.a. at F.

3 Trichloromonofluoromethane has a vapor pressure (absolute) of 13.4 p.s.i.a. at 70 F., and 23.9 p.s.i.a. at 100 F.

Deionized water is also used as well as a fragrance.

To make 1 gram of solution, the following weights are preferred:

( 1) Quaternary detergent 2.0 (2) Ethoxylated fatty acid or alcohols 50.0 (3) Organic acid, USP 5.0 (4) Buffering 2.0 (5 Deionized water, sufficient to make 1 gram. (6) Propellant, about 10% of total mixture exclusive of water.

The weights for 1 gram of the solution may be in the following ranges:

Mg. (1) Quaternary detergent 1.5 to 2.5 (2) Ethoxylated fatty acid or alcohols 30 to 60 3) Organic acid and buffering, sufficient to lower pH of mixture to 4.5 to 5 .5. (4) Deionized water, sufficient to bring weight ofmixture to 1 gram. (5 Propellant, 10% of weight of concentrate (mixture exclusive of water).

Mechanism (Covered by application of Samuel G. Berkow, Serial. No.

861,074, filed Dec. 21, 1959, for Hygienic Dispenser Apparatus, now abandoned.)

The container is a plastic-coated shatter-proof glass bottle. On the stem-valve of this bottle a special ejector fits snugly. The aerosol propellant ejects the above-described solution at a constant, pre-set, safe pressure.

The ejector consists of a nozzle 1 /2 inches in length, a cone which limits the penetration of the nozzle into the vagina to this length, and an adapter by which it is attachedto and activates the stem-valve of the aerosol bottle.

In the forward end of the nozzle there are four openings. An adaptorat the junction of the nozzle and the cone, fits on the stem-valve easily and firmly. Pressure on any side of the cone opens the valve and the solution is propelled into the vagina in four streams at 45 degree angles and at the pre-set pressure. It has been found that emission for 2 seconds is sufficient for all cleansing purposes in all but the most capacious vaginas, in which 3 seconds of fluid-emission may be required. The shortness of the nozzle and angulation of the streams diminish the chance of the cervical intromission of the fluid.

The entire. ejector is easily removed. Made of polypropylene, a plastic only recently available, it can be sterilized by autoclaving or by boiling. Cold sterilization in antiseptic solutions may be employed where necessary.

Uses

This solution and modality has been tested as a replacement for the vaginal douche, in the following conditions: (1) Pre-operative, before vaginal surgery and total hysterectomy, and before such oflice procedures as uterotubal insufilation.

(2) Post-operative, particularly after cervical cauterization and conization.

Results Bacteriologic studies on this preparation were made in vivo and in vitro. It may be emphasized here that the following organisms, obtained from vaginal cultures, were sensitive to our douche solution: Gamma streptococcus, Pseudomonas vulgaris, Aerobacter aerogencs, Staphylococcus albus; whereas B. acidophilus (Doderleins bacillus) was only slightly sensitive to resistant.

Clinical tests indicate the usefulness of this product in vaginal preparation for pelvic surgery. Vaginal cleansing was especially noted on opening the vagina in abdominal hysterectomies. Post-operatively it was used after cervical conization, apparently decreasing the slough and the malodorous discharge.

The ofiice use of this douch solution gave highly satisfactory results whenever vaginal cleansing was desired. There were no untoward effects.

Self-administration by patients proved effective in nonspecific and senile vaginitis. It was useful in conjunction with more specific therapy for trichomonal and monilial vaginitis. The fact that, unlike the vaginal douche, this aerosol preparation can be instilled in bed with a folded towel under the patients hips, without spillage or staining, and the fact that it requires only one or two seconds to administer accounts to some extent for the high degree of patient acceptance.

Summary and conclusions A combination of chemical and physical modalities is offered as a replacement for the vaginal douche.

This solution penetrates into the crevices between the vaginal rugae. It adheres long enough for its medication to be effective.

It is ejected in four angulated streams at a constant preset, safe and effective pressure. The nozzle is short, penetrating the vaginal canal for only 1 /2 inches, so that cervical intromission cannot occur in the normally situated uterus.

The entire procedure takes 2 seconds. It can be satisfactorily performed in bed with a turkish towel folded under hips to catch the small amount of escaping fluid. There is nothing to prepare and nothing to scour or clean, except the plastic ejector which can be sterilized by autoclaving or boiling as well as by cold sterilization.

Bacteriologic studies demonstrate that B. acidophilus is relatively resistant to this preparation, in the concentration of active ingredient employed, whereas Pseudomonas vulgaris, Aerobacter aerogencs, Gamma streptococcus and Staph. albus are sensitive.

As a lubricant and spermaticide, in addition to its cleansing properties the douche solution is satisfactory for use in conjunction with diaphragm contraception, replacing cream or jelly before introduction and the douche previous to removal of the diaphragm.

Present experience justifies the conclusion that this is a safe and effective replacement for the vaginal douche.

What is claimed is:

1. A solution enclosed in a pressurized container comprising a mixture of a cationic quaternary ammonium germicidal surface wetting agent selected from the class consisting of cetyltrimethyl ammonium iodide, cetyltrimethyl ammonium bromide and dimethylbenzyl ammonium chloride, a second wetting agent capable of holding moisture and of serving as an emollient for the first wetting agent and consisting of polyoxyethylene sorbitan monolaurate, a buffered organic acid selected from the class consisting of lactic acid with sodium bicarbonate, citric acid with sodium citrate and acetic acid with sodium acetate, and an nert, non-reactive aerosol propellant comprising tetrafiuorodichloroethane, the ingredients by weight in one gram of the solution being:

(1) cationic quaternary ammonium compound 1.5 to

(2) second wetting agent 30 to 60 mg;

i (3) buffered organic acidsufficient to bring the pH of the mixture down to 4.5 to 5.5;

(4) propellant-about 10% of the mixture weight exclusive of water; and

(5) deionized water sufficient to bring the weight of the mixture to one gram.

2. A solution enclosed in a pressurized container comprising a mixture of a cationic quaternary ammonium germicidal surface wetting agent selected from the class consisting of cetyltrimethyl ammonium iodide, cetyltrimethyl ammonium bromide and dimethylbenzyl ammonium chloride, a second wetting agent capable of holding moisture and of serving as an emollient for the first wetting agent and consisting of polyoxyethylene sorbitan monolaurate, a buffered organic acid selected from the class consisting of lactic acid with sodium bicarbonate, citric acid with sodium citrate and acetic acid with sodium acetate, and an inert, non-reactive aerosol propellant comprising trichloromonofluoromethane, the ingredients by weight in one gram of the solution being:

(1) cationic quaternary ammonium compound 1.5 to

(2) second wetting agent 30 to 60 mg.;

(3) buttered organic acid-sufficient to bring the pH of the mixture down to 4.5 to 5.5;

(4) propellant-about of the mixture weight exclusive of Water; and

(5 deionized Water sufi'icient to bring the weight of the mixture to one gram.

3. A solution enclosed in a pressurized container comprising a mixture of a cationic quaternary ammonium germicidal surface wetting agent selected from the class consisting of cetyltrimethyl ammonium iodide, cetyltrimethyl ammonium bromide and dimethylbenzyl ammonium chloride, a second Wetting agent capable of holding moisture and of serving as an emollient for the first wetting agent and selected from the class consisting of polyoxyethylene sorbitan monolaurate and ethoxylated lanolin alcohols, said ethoxylated lanolin alcohols being derived from sterols and fatty alcohols normally found in skin lipids and cellular tissues of epidermal origin, a buffered organic acid selected from the class consisting of lactic acid with sodium bicarbonate, citric acid with sodium citrate and acetic acid with sodium acetate, and an inert, non-reactive aerosol propellant comprising tetrafluorodichloroethane, the ingredients by weight in one gram of the solution being:

(2) cationic quaternary ammonium compound to (2) second wetting agent to 60 mg.;

(3) buffered organic acidsufiicient to bring the pH of the mixture down to 4.5 to 5.5

(4) propellantabout 10% of the mixture weight ex clusive of water; and

(5 deionized water sufiicient to bring the weight of the mixture to one gram.

4. A solution enclosed in a pressurized container comprising a mixture of a cationic quaternary ammonium germicidal surface wetting agent selected from the class consisting of cetyltrimethyl ammonium iodide, cetyltrimethyl ammonium bromide and dimethylbenzyl ammonium chloride, a second wetting agent capable of holding moisture and of serving as an emollient for the first wet ting agent and selected from the class consisting of polyoxyethylene sorbitan monolaurate and ethoxylated lanolin alcohols, said ethoxylated lanolin alcohols being derived from sterols and fatty alcohols normally found in skin lipids and cellular tissues of epidermal origin, a buttered organic acid selected from the class consisting of lactic acid with sodium bicarbonate, citric acid with sodium citrate and acetic acid with sodium acetate, and an inertnon-reactive aerosol propellant comprising trichloromonofluoromethane, the ingredients by Weight in one gram of the solution being:

(1) cationic quaternary ammonium compound 1.5 to

(2) second wetting agent 30 to mg;

(3) buffered organic acid-suflicient to bring the pH of the mixture down to 4.5 to 5.5;

(4) propellant-about 10% of the mixture weight exclusive of water; and

(5) deionized Water sufficient to bring the Weight of the mixture to one gram.

References Cited by the Examiner UNITED STATES PATENTS 7/1957 Kipnis l67-58.4 9/1958 Elias 167-58 OTHER REFERENCES LEWIS GOTTS, Primary Examiner. FRANK CACCIAPAGLIA, JR., Examiner. 

1. A SOLUTION ENCLOSED IN A PRESURIZED CONTAINTER COMPRISING A MIXTURE OF A CATIONIC QUATERNARY AMMONIUM GERMICIDAL SURFACE WETTING AGENT SELECTED FROM THE CLASS CONSISTING OF CETYLTRIMETHYL AMMONIUM IODIDE, CETYLTRIMETHYL AMMONIUM BROMIDE AND DIMETHYLBENZYL AMMONIUM CHLORIDE, A SECOND WETTING AGENT CAPABLE OF HOLDING MOISTURE AND OF SERVING AS AN EMOLLIENT FOR THE FIRST WETTING AGENT AND CONSISTING OF POLYOXYETHYLENE SORBITAN MONOLAURAE, A BUFFERED ORGANIC ACID SELECTED FROM THE CLASS CONSISTING OF LACTIC ACID WITH SODIUM BICARBONATE, CITRIC ACID WITH SODIUM CITRATE AND ACETIC ACID WITH SODIUM ACETATE, AND AN NERT, NON-REACTIVE AEROSOL PROPELLENT COMPRISING TETRAFLUORODICHLOROETHANE, THE INGREDIENTS BY WEIGHT IN ONE GRAM OF THE SOLUTION BEING: (1) CATIONIC QUATERNARY AMMONIUM COMPOUND 1.5 TO 2.5 MG.; (2) SECOND WETTING AGENT 30 TO 60 MG.; (3) BUFFERED ORGANIC ACID-SUFFICIENT TO BRING THE PH OF THE MIXTURE DOWN TO 4.5 TO 5.5; (4) PROPELLANT-ABOUT 10% OF THE MIXTURE WEIGHT EXCLUSIVE OF WATER; AND (5) DEIONIZED WATER SUFFICIENT TO BRING THE WEIGHT OF THE MIXTURE TO ONE GRAM. 